Pharmacological properties
Terazosin (2- [4-tetrahydrofuranylcarbonyl) -1-piperazinyl] -6,7-dimethoxy-4-quinazolinamine monohydrochloride dihydrate). Terazosin is a selective α1-adrenoceptor blocker. Its antihypertensive effect is due to the blockade of postsynaptic α1-adrenoceptors, which leads to vasodilation, a decrease in OPSS and a decrease in venous return. Terazosin is a long-acting drug, which allows it to be prescribed for hypertension once a day. Long-term treatment is not accompanied by the development of reflex tachycardia; it has a slight effect on cardiac output, renal perfusion and glomerular filtration rate. The drug also increases the rate of urine outflow and reduces obstruction to its outflow. This leads to an improvement in urodynamics in patients with benign prostatic hyperplasia (BPH). The drug does not affect the size of the prostate gland.
Terazosin is rapidly and almost completely absorbed from the gastrointestinal tract after oral administration. Its bioavailability is 90%, the onset of action is 15 minutes after administration. The maximum concentration of the drug in the blood plasma is reached 1 hour after administration. The therapeutic effect develops 2-3 hours later. The antihypertensive effect persists for 24 hours after administration of the drug. Terazosin binds to plasma proteins by 90-94%. It is extensively metabolized in the liver by hydrolysis, demethylation and dealkylation with the formation of 5 different metabolites. The half-life is 12 hours and practically does not change with impaired renal function. Approximately 10 and 20% of the dose taken are excreted unchanged in the urine and feces.
Indication
Treatment of hypertension (as monotherapy and in combination with other antihypertensive agents); symptomatic therapy of BPH.
Application
Ah
The initial daily dose is 1 mg once a day at night. It is recommended to increase the daily dose gradually, doubling it at weekly intervals until the desired effect is achieved. The maintenance dose is 1-5 mg once a day.
BPH
The initial daily dose is 1 mg once a day at night. The maintenance dose is 5-10 mg once a day. The maximum daily dose is 20 mg.
Patients with renal insufficiency and the elderly do not require dose adjustment. Tablets should be taken without chewing, regardless of meals. The drug is not recommended for children.
Contraindication
Hypersensitivity to terazosin or other components of the drug.
Side effects
Dizziness, in severe cases - collapse. To avoid this, it is recommended to start treatment with the drug at a dose of 1 mg at night. Orthostatic hypotension, dizziness, general weakness, edema may occur when using the drug in high doses. Tachycardia, angina pectoris, visual impairment, nausea, vomiting, nasal congestion, digestive tract disorders, decreased libido and impotence, drowsiness, anaphylactic reactions are possible.
Special instructions
At the beginning of treatment, the effect of the first dose may occur - a sharp decrease in blood pressure, dizziness, impaired coordination of movements, loss of consciousness. Similar phenomena may also occur when the drug is resumed after a break in treatment for several days. In such cases, the drug should be prescribed in a dose of 1 mg. Dizziness, impaired coordination of movements often occur when moving from a sitting and lying position to a vertical one. With caution, Setegis tablets should be prescribed to patients with a tendency to develop orthostatic hypotension, as well as to patients with coronary artery disease, other heart diseases, cerebrovascular disorders, hypertensive retinopathy of the III-IV degree.
Before starting treatment for BPH, prostate cancer must be ruled out.
Patients should have their blood pressure monitored at the start of treatment and when changing the dose of the drug. The effectiveness of BPH treatment should be assessed after 4-6 weeks of treatment.
The lactose content in each tablet of Setegis should be taken into account in case of lactase deficiency, galactosemia or glucose/galactose malabsorption syndrome. In 1 tablet 1 mg - 55.0 mg; 2 mg; 5 mg; 10 mg - 110 mg of lactose.
At the initial stage of using Setegis and after each dose increase, you should refrain from performing potentially hazardous activities that require concentration, including driving vehicles.
Interactions
The drug should be prescribed with caution simultaneously with other antihypertensive agents. It is recommended to reduce the dose of the drug when including diuretics or other antihypertensive drugs in the treatment regimen.
If necessary, it is advisable to prescribe another antihypertensive drug in parallel in a low dose under the supervision of a physician.
Overdose
Symptoms: severe hypotension and circulatory failure.
Treatment: the patient should be placed in a horizontal position with the lower extremities elevated. The BCC should be replenished with plasma-replacing solutions, vasopressors should be administered, and electrolyte imbalance should be corrected. Dialysis may be ineffective, as terazosin is highly bound to plasma proteins.
Storage conditions
At a temperature of 15-30 °C.
